United States Patent 10,751,349: Obeticholic Acid Tablet Claims, Expiration, Litigation Risk, and Patent Landscape

U.S. Patent No. 10,751,349 protects a narrowly defined obeticholic acid tablet formulation. The independent claims require four principal elements: obeticholic acid at 1 mg to 50 mg, jet-milled particles below specified size thresholds, a tablet dosage form, and an excipient with a low primary-alcohol impurity level. Claim 19 narrows the excipient requirement to sodium starch glycolate.

The patent does not broadly cover obeticholic acid, all obeticholic acid tablets, or all micronized obeticholic acid products. Its commercial relevance depends on whether a competing product uses jet milling, falls within the claimed particle-size distribution, contains sodium starch glycolate or another qualifying excipient, and uses a formulation process that produces the claimed tablet architecture.

What does U.S. Patent 10,751,349 protect?

U.S. Patent 10,751,349 protects pharmaceutical tablets containing obeticholic acid, also known as OCA, with controlled particle size and excipient impurity specifications.

The broadest independent claim, claim 1, requires:

Claim element	Requirement
Dosage form	Tablet
Active ingredient	Obeticholic acid
OCA quantity	1 mg to 50 mg
Particle production	Jet-milled particles
Maximum particle diameter	Less than about 100 micrometers by laser diffraction
Median particle size	D50 of no more than 50 micrometers
Excipient quality	Total primary alcohol impurity below about 6% by weight

Claim 19 creates a separate independent claim directed specifically to sodium starch glycolate. It requires the same OCA dosage and particle-size limitations but replaces the general excipient requirement with sodium starch glycolate containing less than about 6% total alcohol impurity.

The claims are formulation claims, not composition-of-matter claims to the OCA molecule. They are also not directed solely to a manufacturing process. The phrase "jet-milled particles" is a product limitation tied to the physical characteristics and production history of the active ingredient.

How broad are the independent claims?

Claim 1 is commercially broader than claim 19 because it does not require sodium starch glycolate. It can potentially cover tablets using another pharmaceutically acceptable excipient if that excipient meets the primary-alcohol impurity threshold.

Claim 19 is narrower in excipient identity but may be easier to assess in a product comparison because sodium starch glycolate can be identified from the label, formulation disclosure, supplier documentation, or discovery records.

The principal scope limitations are:

The product must be a tablet.
OCA must be present at a dose from 1 mg through 50 mg.
The OCA must be jet milled.
The particle-size distribution must satisfy the laser-diffraction limitations.
At least one qualifying excipient must meet the impurity threshold under claim 1.
Sodium starch glycolate must meet the impurity threshold under claim 19.

A product containing 5 mg, 10 mg, or 25 mg of OCA is expressly covered by dependent claims 13, 14, and 15 if the other limitations are met. The claims also encompass other dosages within the 1 mg to 50 mg range.

What do the dependent claims add?

The dependent claims progressively narrow particle size, tablet structure, excipient selection, dose, and formulation ratios.

Claims	Added limitation
2	D50 no more than 20 micrometers
3	D50 no more than 10 micrometers
4	Intra-granular and extra-granular portions
5	Extra-granular portion contains no OCA
6	Qualifying excipient is sodium starch glycolate
7	Listed diluents in intra-granular portion
8	Listed diluents in extra-granular portion
9	Diluent is microcrystalline cellulose
10	Microcrystalline cellulose-to-OCA ratio of about 20:1 to 1:5
11	Ratio of about 20:1 to about 1:1
12	Ratio of 20:1 to about 5:1
13	5 mg OCA tablet
14	10 mg OCA tablet
15	25 mg OCA tablet
16	Primary alcohol impurity below about 3%
17	Primary alcohol impurity below about 0.5%
18	D50 no more than 5 micrometers
20	Claim 19 with D50 no more than 5 micrometers
21	Claim 19 with alcohol impurity below about 3%
22	Claim 19 with alcohol impurity below about 0.5%

Claims 4 and 5 are important for manufacturing and formulation analysis. They require a granulated tablet with OCA in the intra-granular portion and excipients outside the granules. Claim 5 excludes OCA from the extra-granular portion.

Claims 9 through 12 create a narrower protection layer around microcrystalline cellulose. The ratio limitations may become significant in an infringement analysis because a product could use the same ingredients but fall outside the claimed ratio.

What is the technical significance of the particle-size limitations?

The patent requires OCA particles produced by jet milling with a D50 value no greater than 50 micrometers. Claims 3 and 18 narrow the median particle size to no more than 10 and 5 micrometers, respectively.

D50 is the particle diameter at which 50% of the measured particle population is smaller and 50% is larger. The claims specify laser diffraction as the analytical method. That measurement method matters because particle-size results can vary based on dispersion conditions, refractive-index assumptions, sample preparation, and instrument settings.

The claim contains two separate particle-size concepts:

Every measured particle must have a diameter below about 100 micrometers.
The median particle size must be at or below the applicable D50 threshold.

A formulation could satisfy the D50 limitation while containing a small fraction of larger particles. The separate "less than about 100 micrometers" limitation therefore creates an additional infringement issue.

"Jet-milled" is also significant. A competitor may argue that a product with the same particle-size profile does not infringe if the particles were produced by a different process, such as wet milling, rotor-stator milling, ball milling, or another micronization technique. The strength of that argument would depend on claim construction, prosecution history, and whether the process term is treated as limiting the claimed product.

What formulations are protected by the patent?

The strongest direct coverage applies to tablets with the following profile:

5 mg, 10 mg, or 25 mg of OCA;
jet-milled OCA;
D50 of no more than 50 micrometers;
sodium starch glycolate;
primary alcohol impurity below 6%;
microcrystalline cellulose in the intra-granular portion;
no OCA in the extra-granular portion; and
a microcrystalline cellulose-to-OCA ratio within the claimed range.

The patent also covers broader combinations using other listed diluents, including starch, pregelatinized starch, lactose, calcium phosphate, mannitol, sorbitol, sucrose, and related materials.

The impurity limitation is unusual because it focuses on the composition of an excipient rather than only the identity or quantity of the excipient. Claims 16, 17, 21, and 22 provide narrower fallback positions at below 3% and below 0.5%.

When does U.S. Patent 10,751,349 lose exclusivity?

The patent issued on August 25, 2020. Its term is governed by the earliest effective nonprovisional or PCT filing in the relevant priority chain, not simply by the issue date. Based on the patent-family structure associated with this OCA formulation technology, the nominal expiration is projected to fall in 2035, subject to patent-term adjustment, patent-term extension, terminal disclaimers, and the specific priority record shown in USPTO Patent Center.

Event	Date or status
Patent	U.S. 10,751,349
Issue date	August 25, 2020
Technology	OCA tablet formulation and particle-size control
Nominal term basis	20 years from earliest effective application filing
Projected term period	2035, subject to adjustment
Regulatory exclusivity	Separate from patent term
Orange Book impact	Depends on FDA listing and listed use

The patent term should not be confused with Ocaliva's FDA regulatory exclusivity. Ocaliva received FDA approval for primary biliary cholangitis in 2016. Regulatory exclusivity periods are shorter than the projected patent term and do not independently determine whether a generic can launch after approval.

What is the Orange Book status of U.S. Patent 10,751,349?

The Orange Book is the controlling FDA source for determining whether a patent is listed against an approved drug product, the listed patent use code, and the applicable patent expiration information. A patent directed to a drug product formulation may be eligible for listing if it meets FDA's patent-listing criteria.

For Ocaliva, the commercial significance of U.S. 10,751,349 depends on:

whether the patent is listed against the approved OCA product;
whether the listing covers the approved tablet strengths;
whether a use code limits the listed scope;
whether the patent is challenged in an ANDA certification; and
whether the listing remains active or has been delisted.

An Orange Book listing does not establish validity or infringement. It creates procedural consequences for an ANDA applicant, including the possibility of a Paragraph IV certification and a 30-month stay if the patent owner brings timely litigation. FDA, Approved Drug Products with Therapeutic Equivalence Evaluations, is the primary source for current listing data.[1]

What Paragraph IV challenges and generic entry risks exist?

A generic applicant seeking approval before expiration may submit a Paragraph IV certification asserting that the patent is invalid, unenforceable, or not infringed. For this patent, the most likely technical positions would focus on the following limitations:

Particle-size and milling challenges

An applicant may contend that its OCA is not jet milled, does not meet the D50 requirement, or contains particles above the claimed maximum. Testing methodology would be central. The applicant would need to establish the particle-size profile under defensible laser-diffraction conditions.

Excipient impurity challenges

The applicant may use an excipient with a primary-alcohol impurity level at or above the claimed threshold, or challenge whether the claimed impurity measurement is definite and reproducible.

Product-by-process issues

The phrase "jet-milled particles" could support a noninfringement argument based on the actual manufacturing route. The patent owner could respond that the process limitation identifies a product having a distinctive particle-size profile or that the accused particles are in fact produced through jet milling at a relevant manufacturing stage.

Formulation architecture

A competitor may place all excipients in a single blend, include OCA in the extra-granular portion, or use a formulation that does not contain the claimed intra-granular/extra-granular structure. Such changes would matter primarily for claims 4, 5, and 7 through 12.

How can a competitor design around the patent?

Potential design-around paths include:

Design strategy	Claim limitation targeted
Use a non-tablet dosage form	Tablet requirement
Use a different milling process	"Jet-milled" limitation
Use OCA with D50 above 50 micrometers	D50 limitation
Use a particle population exceeding the claimed size profile	Less-than-100-micrometer limitation
Use an excipient outside the claimed impurity threshold	Alcohol impurity limitation
Avoid sodium starch glycolate	Claims 6 and 19 through 22
Put OCA in the extra-granular portion	Claims 4 and 5
Use a different diluent	Claims 7 through 12
Use a different microcrystalline cellulose ratio	Claims 10 through 12
Use a capsule, suspension, or other dosage form	Tablet limitation

These are only literal-scope design considerations. The doctrine of equivalents could create residual risk where a substitute performs substantially the same function in substantially the same way to achieve substantially the same result. Prosecution-history estoppel may limit that risk if the patent owner narrowed the claims to obtain allowance.

How strong is the patent estate for obeticholic acid?

U.S. 10,751,349 is strongest as a formulation patent and weaker as a standalone barrier to all generic OCA products.

Estate component	Relative significance
OCA molecule	Not covered by this patent
OCA tablet	Covered only if the listed limitations are met
Jet-milled OCA	Central technical limitation
Sodium starch glycolate	Specifically protected in claim 19
Granulated tablet structure	Protected in dependent claims
5 mg, 10 mg, 25 mg strengths	Expressly covered
Method of treatment	Not claimed in the provided claims
Manufacturing method	Not claimed as a standalone process
Injectable or capsule products	Outside the literal tablet claims

The estate's practical strength increases if companion patents cover the active ingredient's therapeutic use, additional formulations, manufacturing processes, or approved product presentations. It decreases if competitors can obtain the same clinical and bioequivalence profile without using jet-milled OCA or the claimed excipient specifications.

What patent litigation or settlements affect this patent?

The supplied claims do not establish whether U.S. 10,751,349 has been asserted, challenged, invalidated, disclaimed, or resolved through settlement. Patent litigation status must be determined from PACER, the USPTO Patent Center file history, district-court dockets, and any Federal Circuit decisions.

For an ANDA challenge, the relevant procedural events would include:

Paragraph IV certification;
notice to the patent owner and NDA holder;
infringement complaint within the statutory period;
possible 30-month FDA stay;
claim-construction and validity proceedings;
settlement or consent judgment; and
final FDA approval timing.

A settlement may permit an authorized generic, a delayed generic launch, a license, or a launch date before patent expiration. The patent number alone does not reveal those commercial terms.

How does this patent compare with method-of-use and molecule patents?

U.S. 10,751,349 has a different risk profile from OCA composition-of-matter and method-of-use patents.

Patent category	Primary barrier	Typical generic exposure
Composition of matter	OCA molecule or chemical class	Broadest
Method of use	Treatment of a specified disease or population	Depends on label and skinny-label strategy
Formulation	Tablet composition and manufacturing attributes	Product-specific
Manufacturing process	Production route or purification	Process-specific
U.S. 10,751,349	Jet-milled OCA tablet with low-impurity excipient	Narrower but technically testable

A generic product can avoid this patent while still facing other Orange Book-listed patents. Conversely, avoiding this patent does not remove the need to assess OCA use patents, polymorphs, salt forms, dosage regimens, and other formulation patents in the family.

What is the commercial exposure from this patent?

The principal commercial exposure concerns generic versions of Ocaliva tablets at the approved strengths, particularly 5 mg and 10 mg products. Claim 15 also expressly covers 25 mg tablets, although the commercial importance of that strength depends on the approved product and market demand.

The patent creates a risk of:

delayed ANDA approval;
Paragraph IV litigation;
formulation reformulation costs;
additional analytical testing;
manufacturing-process changes;
loss of launch flexibility;
potential damages or injunction exposure; and
licensing costs.

Its commercial leverage is highest if OCA tablets using jet-milled material and sodium starch glycolate are the most practical route to bioequivalence. Its leverage is lower if alternative particle-engineering and excipient combinations achieve the required dissolution and exposure profile.

Key Takeaways

U.S. 10,751,349 is a formulation patent, not a broad patent on obeticholic acid.
Claim 1 requires a tablet, 1 mg to 50 mg of OCA, jet-milled particles, D50 no greater than 50 micrometers, and an excipient with less than about 6% primary alcohol impurity.
Claim 19 specifically targets sodium starch glycolate with the same impurity threshold.
Claims 18 and 20 create narrower protection for OCA with a D50 of no more than 5 micrometers.
Claims 4 and 5 protect a granulated architecture in which OCA is intra-granular and absent from the extra-granular portion.
Claims 13 through 15 expressly cover 5 mg, 10 mg, and 25 mg tablets.
The projected patent term extends into 2035, subject to the USPTO term calculation and any adjustment or disclaimer.
Key generic defenses involve non-jet-milled OCA, different particle-size profiles, alternative excipients, different granulation architecture, and different microcrystalline cellulose ratios.
Orange Book listing, Paragraph IV activity, litigation, and settlement terms require review of current FDA and court records.
The patent is commercially meaningful but should be analyzed as one layer of a broader OCA patent estate.

FAQs About U.S. Patent 10,751,349

Does U.S. Patent 10,751,349 cover all Ocaliva tablets?

No. It covers only tablets meeting the combined OCA dose, jet-milled particle-size, and excipient impurity limitations.

Does the patent cover obeticholic acid capsules?

No. The provided claims require a tablet. A capsule would not literally satisfy that dosage-form limitation.

Is sodium starch glycolate required in every claim?

No. It is required by claim 6 and independent claim 19, but claim 1 covers a broader class of qualifying pharmaceutically acceptable excipients.

Can a generic use micronized obeticholic acid without infringing?

Possibly. The analysis would depend on whether the particles were jet milled and whether the measured particle-size distribution satisfies the claims. Micronization alone does not establish infringement.

Does FDA approval of a generic automatically eliminate this patent risk?

No. FDA approval and patent infringement are separate issues. An ANDA applicant may need to resolve an Orange Book-listed patent through a Paragraph IV certification, litigation, settlement, or expiration.

References

U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations. FDA.
United States Patent and Trademark Office. (2020). U.S. Patent No. 10,751,349. USPTO.
U.S. Food and Drug Administration. (2016). Ocaliva prescribing information. FDA.
United States Code. (2024). 35 U.S.C. §§ 154, 271, and 355. U.S. Government Publishing Office.
U.S. Food and Drug Administration. (2024). ANDA submissions: Content, format, and review. FDA.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Intercept	OCALIVA	obeticholic acid	TABLET;ORAL	207999-001	May 27, 2016		DISCN	Yes	No	10,751,349	⤷ Start Trial	Y				⤷ Start Trial
Intercept	OCALIVA	obeticholic acid	TABLET;ORAL	207999-002	May 27, 2016		DISCN	Yes	No	10,751,349	⤷ Start Trial	Y				⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	104427	⤷ Start Trial
Australia	2016255045	⤷ Start Trial
Australia	2020205315	⤷ Start Trial
Brazil	112017023161	⤷ Start Trial
Canada	2983609	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 10,751,349

Which drugs does patent 10,751,349 protect, and when does it expire?

Summary for Patent: 10,751,349